DOVER, Del., April 4, 2024. Eilean Therapeutics LLC, a biopharmaceutical company dedicated to discovering and developing best-in-class and first-in-class small molecule inhibitors to target escape mutations in hematologic and solid malignancies, is pleased to announce the clearance from the Human Research Ethics Committee in Australia for lomonitinib (ZE46-0134) allowing the company to proceed with a Phase I clinical trial in relapsed/refractory (R/R) AML.

多佛，Del。，2024年4月4日。Eilean Therapeutics LLC是一家生物制药公司，致力于发现和开发一流和一流的小分子抑制剂，以靶向血液学和实体恶性肿瘤中的逃逸突变，很高兴宣布澳大利亚人类研究伦理委员会批准洛莫替尼（ZE46-0134），允许该公司进行复发/难治性（R/R）AML的I期临床试验。

Lomonitinib is a highly potent and selective plan-FLT3/IRAK4 inhibitor that targets clinically relevant FLT3 mutations and putative escape pathways.'This is a major milestone for the Eilean team, as we continue to progress the accelerated development of lomonitinib,' stated Iain Dukes, CEO of Eilean Therapeutics.

洛莫替尼是一种高效且选择性的plan-FLT3/IRAK4抑制剂，可靶向临床相关的FLT3突变和推定的逃逸途径。”Eilean Therapeutics首席执行官伊恩·杜克斯（IainDukes）表示，这是Eilean团队的一个重要里程碑，因为我们继续推进洛莫尼尼的加速开发。

'Given the safety profile, extended half-life and target engagement demonstrated in a healthy volunteer study, we look forward to initiating our clinical trial and testing our approach in R/R AML patients.'About LomonitinibLomonitinib is a highly potent and selective inhibitor of FLT3 ITD, TKD and other clinically relevant FLT3 mutations, as well as IRAK4.

“鉴于健康志愿者研究显示的安全性，延长半衰期和目标参与度，我们期待着启动我们的临床试验，并在R/R AML患者中测试我们的方法。”关于LomonitinibLomonitinib是FLT3 ITD，TKD和其他临床相关FLT3突变以及IRAK4的高效选择性抑制剂。

FLT3 mutations are the most frequently identified mutations in AML. There are two main mechanisms of resistance to FLT3 inhibitors: the FLT3-ITD-F691L mutation deemed the 'gatekeeper' mutation that confers resistance to all currently approved FLT3 inhibitors and the activation of the IRAK4 escape pathway.

FLT3突变是AML中最常见的突变。对FLT3抑制剂的抗性有两种主要机制：FLT3-ITD-F691L突变被认为是“看门人”突变，赋予对所有目前批准的FLT3抑制剂的抗性和IRAK4逃逸途径的激活。

Lomonitinib inhibits both resistance mechanisms.About the Phase 1 Clinical TrialThe Phase I study will evaluate the safety, tolerability, pharmacokinetics, and anti-tumor activity of lomonitinib as monotherapy in R/R AML patients with FLT3 mutations (ITD, TKD or gatekeeper). The study will include a dose escalation and an expansion phase with up to 60 tota.

洛莫替尼抑制两种耐药机制。关于1期临床试验I期研究将评估洛莫替尼作为FLT3突变（ITD，TKD或gatekeeper）的R/R AML患者单药治疗的安全性，耐受性，药代动力学和抗肿瘤活性。该研究将包括剂量递增和扩展阶段，最高可达60 tota。